Open Access
ARTICLE
Experimental and In Silico Analysis of Cordycepin and its Derivatives as Endometrial Cancer Treatment
Pedro Fong*1,
Cheng N. Ao*†1,
Kai I. Tou*, Ka M. Huang*, Chi C. Cheong*, Li R. Meng*
* School of Health Sciences, Macao Polytechnic Institute, Macao, P.R. China
† State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology,
Macao, P.R. China
Oncology Research 2019, 27(2), 237-251. https://doi.org/10.3727/096504018X15235274183790
Abstract
The aim of this study was to investigate the inhibition effects of cordycepin and its derivatives on endometrial
cancer cell growth. Cytotoxicity MTT assays, clonogenic assays, and flow cytometry were used to observe
the effects on apoptosis and regulation of the cell cycle of Ishikawa cells under various concentrations of
cordycepin, cisplatin, and combinations of the two. Validated in silico docking simulations were performed
on 31 cordycepin derivatives against adenosine deaminase (ADA) to predict their binding affinities and hence
their potential tendency to be metabolized by ADA. Cordycepin has a significant dose-dependent inhibitory
effect on cell proliferation. The combination of cordycepin and cisplatin produced greater inhibition effects
than did cordycepin alone. Apoptosis investigations confirmed the ability of cordycepin to induce the apoptosis of Ishikawa cells. The in silico results indicate that compound MRS5698 is least metabolized by ADA
and has acceptable drug likeness and safety profiles. This is the first study to confirm the cytotoxic effects of
cordycepin on endometrial cancer cells. This study also identified cordycepin derivatives with promising pharmacological and pharmacokinetic properties for further investigation in the development of new treatments for
endometrial cancer
Keywords
Cite This Article
Fong, P., Cheng,
., Kai,
., Huang, K. M., Cheong, C. C. et al. (2019). Experimental and In Silico Analysis of Cordycepin and its Derivatives as Endometrial Cancer Treatment.
Oncology Research, 27(2), 237–251.